메뉴 건너뛰기




Volumn 23, Issue 1, 2014, Pages 55-66

Update on the status of DP2 receptor antagonists; From proof of concept through clinical failures to promising new drugs

Author keywords

ADC 3680; ARRY 502; Asthma; BI 671800; DP1 receptor; DP2 receptor; Eosinophil; Inflammation; MK 1029; OC 459; PGD2; Setipiprant; Vidupiprant

Indexed keywords

ADC 3680; AM 211; AM 461; ARRY 502; ASP 5642; ATX 2417; AZD 1981; AZD 5985; AZD 8075; BI 144807; BI 671800; CETIRIZINE; CORTICOSTEROID; FLUTICASONE PROPIONATE; KETOCONAZOLE; MK 1029; MK 7246; MOMETASONE FUROATE; MONTELUKAST; NEW DRUG; OC 459; ONO 4053; PROSTAGLANDIN RECEPTOR BLOCKING AGENT; QAV 680; QAW 039; RG 7185; SETIPIPRANT; TM 30089; UNCLASSIFIED DRUG; VIDUPIPRANT;

EID: 84889841360     PISSN: 13543784     EISSN: 17447658     Source Type: Journal    
DOI: 10.1517/13543784.2013.839658     Document Type: Review
Times cited : (39)

References (67)
  • 1
    • 0018071995 scopus 로고
    • Characterization of the reaction sequence involved in phospholipid labeling and deacylation and prostaglandin synthesis and actions
    • DOI 10.1016/0091-6749(78)90085-4
    • Needleman P. Characterization of the reaction sequence involved in phospholipid labeling and deacylation and prostaglandin synthesis and actions. J Allergy Clin Immunol 1978;62(2):96-102 (Pubitemid 9003161)
    • (1978) Journal of Allergy and Clinical Immunology , vol.62 , Issue.2 , pp. 96-102
    • Needleman, P.1
  • 2
    • 0024548854 scopus 로고
    • Spectrum of prostanoid release after bronchoalveolar allergen challenge in atopic asthmatics and in control groups. An alteration in the ratio of bronchoconstrictive to bronchoprotective mediators
    • Wenzel SE, Westcott JY, Smith HR, Larsen GL. Spectrum of prostanoid release after bronchoalveolar allergen challenge in atopic asthmatics and in control groups. An alteration in the ratio of bronchoconstrictive to bronchoprotective mediators. Am Rev Respir Dis 1989;139(2):450-7 (Pubitemid 19057424)
    • (1989) American Review of Respiratory Disease , vol.139 , Issue.2 , pp. 450-457
    • Wenzel, S.E.1    Westcott, J.Y.2    Smith, H.R.3    Larsen, G.L.4
  • 3
    • 79955575162 scopus 로고    scopus 로고
    • International union of basic and clinical pharmacology. LXXXIII: Classification of prostanoid receptors, updating 15 years of progress
    • Woodward DF, Jones RL, Narumiya S. International Union of Basic and Clinical Pharmacology. LXXXIII: classification of prostanoid receptors, updating 15 years of progress. Pharmacol Rev 2011;63(3):471-538
    • (2011) Pharmacol Rev , vol.63 , Issue.3 , pp. 471-538
    • Woodward, D.F.1    Jones, R.L.2    Narumiya, S.3
  • 4
    • 0024547972 scopus 로고
    • The classification of prostaglandin DP-receptors in platelets and vasculature using BW A868C, a novel, selective and potent competitive antagonist
    • Giles H, Leff P, Bolofo ML, et al. The classification of prostaglandin DP-receptors in platelets and vasculature using BW A868C, a novel, selective, and potent competitive antagonist. Br J Pharmacol 1989;96:291-300 (Pubitemid 19045102)
    • (1989) British Journal of Pharmacology , vol.96 , Issue.2 , pp. 291-300
    • Giles, H.1    Leff, P.2    Bolofo, M.L.3    Kelly, M.G.4    Robertson, A.D.5
  • 5
    • 0023740545 scopus 로고
    • Characterisation of receptors mediating the contractile effects of prostanoids in guinea-pig and human airways
    • McKenniff MG, Rodger IW, Norman P, Gardiner PJ. Characterisation of receptors mediating the contractile effects of prostanoids in guinea-pig and human airways. Eur J Pharmacol 1988;153(2-3):149-59
    • (1988) Eur J Pharmacol , vol.153 , Issue.2-3 , pp. 149-159
    • McKenniff, M.G.1    Rodger, I.W.2    Norman, P.3    Gardiner, P.J.4
  • 8
    • 0038138607 scopus 로고    scopus 로고
    • 2 receptor CRTH2: Structure, properties, and functions in leukocytes
    • DOI 10.1016/S0952-3278(03)00078-4
    • Nagata K, Hirai H. The second PGD(2) receptor CRTH2: structure, properties, and functions in leukocytes. Prostaglandins Leukot Essent Fatty Acids 2003;69(2-3):169-77 (Pubitemid 36976172)
    • (2003) Prostaglandins Leukotrienes and Essential Fatty Acids , vol.69 , Issue.2-3 , pp. 169-177
    • Nagata, K.1    Hirai, H.2
  • 9
    • 33947726053 scopus 로고    scopus 로고
    • 1 and CRTH2 as an approach to treat allergic diseases
    • DOI 10.1038/nrd2266, PII NRD2266
    • Pettipher R, Hansel TT, Armer R. Antagonism of the prostaglandin D2 receptors DP1 and CRTH2 as an approach to treat allergic diseases. Nat Rev Drug Discov 2007;6(4):313-25 (Pubitemid 46505882)
    • (2007) Nature Reviews Drug Discovery , vol.6 , Issue.4 , pp. 313-325
    • Pettipher, R.1    Hansel, T.T.2    Armer, R.3
  • 11
    • 0025999792 scopus 로고
    • BAY u3405, a potent and selective thromboxane A2 receptor antagonist on airway smooth muscle in vitro
    • McKenniff MG, Norman P, Cuthbert NJ, Gardiner PJ. BAY u3405, a potent and selective thromboxane A2 receptor antagonist on airway smooth muscle in vitro. Br J Pharmacol 1991;104(3):585-90
    • (1991) Br J Pharmacol , vol.104 , Issue.3 , pp. 585-590
    • McKenniff, M.G.1    Norman, P.2    Cuthbert, N.J.3    Gardiner, P.J.4
  • 12
    • 0026683661 scopus 로고
    • Effects of a thromboxane-receptor antagonist, BAY u 3405, on prostaglandin D2-and exercise-induced bronchoconstriction
    • Magnussen H, Boerger S, Templin K, Baunack AR. Effects of a thromboxane-receptor antagonist, BAY u 3405, on prostaglandin D2-and exercise-induced bronchoconstriction. J Allergy Clin Immunol 1992;89(6):1119-26
    • (1992) J Allergy Clin Immunol , vol.89 , Issue.6 , pp. 1119-1126
    • Magnussen, H.1    Boerger, S.2    Templin, K.3    Baunack, A.R.4
  • 13
    • 22744445889 scopus 로고    scopus 로고
    • Small-molecule CRTH2 antagonists for the treatment of allergic inflammation: An overview
    • DOI 10.1517/13543784.14.7.769
    • Ly TW, Bacon KB. Small-molecule CRTH2 antagonists for the treatment of allergic inflammation: an overview. Expert Opin Investig Drugs 2005;14(7):769-73 (Pubitemid 41030945)
    • (2005) Expert Opinion on Investigational Drugs , vol.14 , Issue.7 , pp. 769-773
    • Ly, T.W.1    Bacon, K.B.2
  • 14
    • 77954725559 scopus 로고    scopus 로고
    • DP2 receptor antagonists in development
    • Norman P. DP2 Receptor Antagonists in Development. Expert Opin Investig Drugs 2010;19(8):947-61
    • (2010) Expert Opin Investig Drugs , vol.19 , Issue.8 , pp. 947-961
    • Norman, P.1
  • 15
    • 84859787191 scopus 로고    scopus 로고
    • Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). from lead optimization to clinical proof-of-concept in asthma and allergic rhinitis
    • Pettipher R, Whittaker M. Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis. J Med Chem 2012;55(7):2915-31
    • (2012) J Med Chem , vol.55 , Issue.7 , pp. 2915-2931
    • Pettipher, R.1    Whittaker, M.2
  • 16
    • 84871483728 scopus 로고    scopus 로고
    • Novel prostaglandin receptor modulators: A patent review 2002-2012)-part I: Non-EP receptor modulators
    • Lamers C, Flesch D, Schubert-Zsilavecz M, Merk D. Novel prostaglandin receptor modulators: a patent review (2002-2012)-part I: non-EP receptor modulators. Expert Opin Ther Pat 2013;23(1):47-77
    • (2013) Expert Opin Ther Pat , vol.23 , Issue.1 , pp. 47-77
    • Lamers, C.1    Flesch, D.2    Schubert-Zsilavecz, M.3    Merk, D.4
  • 17
    • 84889799394 scopus 로고    scopus 로고
    • Efficacy and safety of BI 671800, an oral CRTH2 antagonist, as add on therapy in poorly controlled asthma patients prescribed an inhaled corticosteroid
    • Hall I, Sarno M, Diss B, et al. Efficacy and safety of BI 671800, an oral CRTH2 antagonist, as add on therapy in poorly controlled asthma patients prescribed an inhaled corticosteroid. European Resp J 2012;P1792
    • (2012) European Resp J
    • Hall, I.1    Sarno, M.2    Diss, B.3
  • 18
    • 84889764409 scopus 로고    scopus 로고
    • Efficacy and safety of BI 671800, an oral CRTH2 antagonist in controller näve patients with poorly-controlled asthma
    • Sutherland R, Tetzlaff K, Nivens C, et al. Efficacy and safety of BI 671800, an oral CRTH2 antagonist in controller näve patients with poorly-controlled asthma. European Resp J 2012;P3084
    • (2012) European Resp J
    • Sutherland, R.1    Tetzlaff, K.2    Nivens, C.3
  • 19
    • 84889799394 scopus 로고    scopus 로고
    • Efficacy and safety of BI 671800, an oral CRTH2 antagonist, as add on therapy in poorly controlled asthma patients prescribed an inhaled corticosteroid
    • Fowler A, Miller C, LaForce D, et al. Efficacy and safety of BI 671800, an oral CRTH2 antagonist, as add on therapy in poorly controlled asthma patients prescribed an inhaled corticosteroid. European Resp J 2012;P3085
    • (2012) European Resp J
    • Fowler, A.1    Miller, C.2    Laforce, D.3
  • 20
    • 84867389374 scopus 로고    scopus 로고
    • CRTH2 Antagonist, BI 671800 (BI), reduces nasal symptoms and inhibits nasal cytokines and eosinophils in SAR patients exposed to grass pollen in an environmental challenge chamber (ECC)
    • Krug N, Gupta A, Badorrek D, et al. CRTH2 Antagonist, BI 671800 (BI), reduces nasal symptoms and inhibits nasal cytokines and eosinophils in SAR patients exposed to grass pollen in an environmental challenge chamber (ECC). Am J Resp Crit Care Med 2012;185:A4185
    • (2012) Am J Resp Crit Care Med , vol.185
    • Krug, N.1    Gupta, A.2    Badorrek, D.3
  • 21
    • 84860697146 scopus 로고    scopus 로고
    • T cell homing to epithelial barriers in allergic disease
    • Islam SA, Luster AD. T cell homing to epithelial barriers in allergic disease. Nat Med 2012;18(5):705-15
    • (2012) Nat Med , vol.18 , Issue.5 , pp. 705-715
    • Islam, S.A.1    Luster, A.D.2
  • 22
    • 84862622198 scopus 로고    scopus 로고
    • UGT2B17 genetic polymorphisms dramatically affect the pharmacokinetics of MK-7246 in healthy subjects in a first-in-human study
    • Wang YH, Trucksis M, McElwee JJ, et al. UGT2B17 genetic polymorphisms dramatically affect the pharmacokinetics of MK-7246 in healthy subjects in a first-in-human study. Clin Pharmacol Ther 2012;92(1):96-102
    • (2012) Clin Pharmacol Ther , vol.92 , Issue.1 , pp. 96-102
    • Wang, Y.H.1    Trucksis, M.2    McElwee, J.J.3
  • 24
    • 78651233023 scopus 로고    scopus 로고
    • Azaindoles as potent CRTH2 receptor antagonists
    • Simard D, Leblanc Y, Berthelette C, et al. Azaindoles as potent CRTH2 receptor antagonists. Bioorg Med Chem Lett 2011;21(2):841-5
    • (2011) Bioorg Med Chem Lett , vol.21 , Issue.2 , pp. 841-845
    • Simard, D.1    Leblanc, Y.2    Berthelette, C.3
  • 25
    • 84889863764 scopus 로고    scopus 로고
    • The in vitro profile of ADC3680, a potent and selective CRTh2 antagonist for the treatment of inadequately controlled Asthma
    • Fitzgerald MF, Whitmarsh M, Prosser J, et al. The In Vitro Profile Of ADC3680, A Potent And Selective CRTh2 Antagonist For The Treatment Of Inadequately Controlled Asthma. Am J Resp Crit Care Med 2013;187:A2617
    • (2013) Am J Resp Crit Care Med , vol.187
    • Fitzgerald, M.F.1    Whitmarsh, M.2    Prosser, J.3
  • 26
    • 84889763595 scopus 로고    scopus 로고
    • The safety, PK and PD Profile of ADC3680, a potent and selective CRTh2 Antagonist, in healthy volunteers and partly controlled atopic asthmatic subjects
    • Fitzgerald MF, Snape S, Febrarro S, et al. The safety, PK and PD Profile Of ADC3680, a potent and selective CRTh2 Antagonist, in healthy volunteers and partly controlled atopic asthmatic subjects. Am J Resp Crit Care Med 2013;187:A3874
    • (2013) Am J Resp Crit Care Med , vol.187
    • Fitzgerald, M.F.1    Snape, S.2    Febrarro, S.3
  • 27
    • 84889850906 scopus 로고    scopus 로고
    • Research Ethics Service 11/WA/0324 Avaiolable from
    • Research Ethics Service. A Study of 14C-ADC3680 in Healthy Volunteers. 11/WA/0324 2011. Avaiolable from http://www.nres.nhs.uk/researchsummaries/ entryid29=137794&q=0~adc3680
    • (2011) A Study of 14C-ADC3680 in Healthy Volunteers
  • 28
    • 84856006564 scopus 로고    scopus 로고
    • Pharmacologic profile of OC000459, a Potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T Helper 2 Lymphocytes and Eosinophils
    • Pettipher R, Vinall SL, Xue L, et al. Pharmacologic profile of OC000459, a Potent, selective, and orally active D prostanoid receptor 2 antagonist that inhibits mast cell-dependent activation of T Helper 2 Lymphocytes and Eosinophils. J Pharmacol Exp Ther 2012;340(2):473-82
    • (2012) J Pharmacol Exp Ther , vol.340 , Issue.2 , pp. 473-482
    • Pettipher, R.1    Vinall, S.L.2    Xue, L.3
  • 29
    • 84655167630 scopus 로고    scopus 로고
    • A randomized double-blind placebo-controlled study of the CRTH2 antagonist OC000459 in moderate persistent asthma
    • Barnes N, Pavord I, Chuchalin A, et al. A randomized, double-blind, placebo-controlled study of the CRTH2 antagonist OC000459 in moderate persistent asthma. Clin Exp Allergy 2012;42(1):38-48
    • (2012) Clin Exp Allergy , vol.42 , Issue.1 , pp. 38-48
    • Barnes, N.1    Pavord, I.2    Chuchalin, A.3
  • 30
    • 84872187666 scopus 로고    scopus 로고
    • Inhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459
    • Singh D, Cadden P, Hunter M, et al. Inhibition of the asthmatic allergen challenge response by the CRTH2 antagonist OC000459. Eur Respir J 2013;41(1):46-52
    • (2013) Eur Respir J , vol.41 , Issue.1 , pp. 46-52
    • Singh, D.1    Cadden, P.2    Hunter, M.3
  • 31
    • 84869495906 scopus 로고    scopus 로고
    • The CRTH2 antagonist OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen a randomised placebo-controlled double-blind trial
    • Horak F, Zieglmayer P, Zieglmayer R, et al. The CRTH2 antagonist OC000459 reduces nasal and ocular symptoms in allergic subjects exposed to grass pollen, a randomised, placebo-controlled, double-blind trial. Allergy 2012;67(12):1572-9
    • (2012) Allergy , vol.67 , Issue.12 , pp. 1572-1579
    • Horak, F.1    Zieglmayer, P.2    Zieglmayer, R.3
  • 32
    • 84889785447 scopus 로고    scopus 로고
    • Array BioPharma Available from [Last accessed 23 July 2013]
    • Array BioPharma. ARRY-502 Meets primary and key secondary endpoints in asthma study. Available from: http://phx. corporate-ir.net/phoenix.zhtml c=123810&p=irolnewsArticle& ID=1839862 [Last accessed 23 July 2013]
    • ARRY-502 Meets Primary and Key Secondary Endpoints in Asthma Study
  • 33
    • 84873708317 scopus 로고    scopus 로고
    • Anti-eosinophil activity and clinical efficacy of the CRTH2 antagonist OC000459 in eosinophilic esophagitis
    • Straumann A, Hoesli S, Bussmann Ch, et al. Anti-eosinophil activity and clinical efficacy of the CRTH2 antagonist OC000459 in eosinophilic esophagitis. Allergy 2013;68(3):375-85
    • (2013) Allergy , vol.68 , Issue.3 , pp. 375-385
    • Straumann, A.1    Hoesli, S.2    Bussmann, C.H.3
  • 35
    • 84889837465 scopus 로고    scopus 로고
    • Safety, PK and PD of ARRY-502, a CRTh2 Antagonist, in Healthy Subjects with a History of Seasonal Allergies
    • Burgess L, Anderson C, Nugent N, et al. Safety, PK and PD of ARRY-502, a CRTh2 Antagonist, in Healthy Subjects with a History of Seasonal Allergies. Inflamm Res 2010;59(suppl 3):S287
    • (2010) Inflamm Res , vol.59 , Issue.SUPPL. 3
    • Burgess, L.1    Anderson, C.2    Nugent, N.3
  • 36
    • 84889841605 scopus 로고    scopus 로고
    • Safety, PK and PD of ARRY-502, a CRTh2 Antagonist, in healthy subjects with a history of seasonal allergies
    • Bell S, Anderson L, Nugent C, et al. Safety, PK and PD of ARRY-502, a CRTh2 Antagonist, in healthy subjects with a history of seasonal allergies. Eur Resp J 2010;36(suppl):708s
    • (2010) Eur Resp J , vol.36 , Issue.SUPPL.
    • Bell, S.1    Anderson, L.2    Nugent, C.3
  • 37
    • 84889780126 scopus 로고    scopus 로고
    • The Signature Selection Strategies for CRTh2 Antagonists: Baseline Characteristics of a Mild to Moderate Persistent Asthma Population
    • Chantry D, Ono J, Eberhardt C, et al. The Signature Selection Strategies for CRTh2 Antagonists: baseline Characteristics of a Mild to Moderate Persistent Asthma Population. Am J Resp Crit Care Med 2013;187:A1339
    • (2013) Am J Resp Crit Care Med , vol.187
    • Chantry, D.1    Ono, J.2    Eberhardt, C.3
  • 38
    • 79959497075 scopus 로고    scopus 로고
    • Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation
    • Bain G, Lorrain DS, Stebbins KJ, et al. Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation. J Pharmacol Exp Ther 2011;338(1):290-301
    • (2011) J Pharmacol Exp Ther , vol.338 , Issue.1 , pp. 290-301
    • Bain, G.1    Lorrain, D.S.2    Stebbins, K.J.3
  • 39
    • 84870409539 scopus 로고    scopus 로고
    • Pharmacodynamics pharmacokinetics, and safety of AM211: A novel and potent antagonist of the prostaglandin D2 receptor type
    • Bain G, King CD, Brittain J, et al. Pharmacodynamics, pharmacokinetics, and safety of AM211: a novel and potent antagonist of the prostaglandin D2 receptor type. J Clin Pharmacol 2012;52(10):1482-93
    • (2012) J Clin Pharmacol , vol.52 , Issue.10 , pp. 1482-1493
    • Bain, G.1    King, C.D.2    Brittain, J.3
  • 40
    • 81855168393 scopus 로고    scopus 로고
    • A novel DP2 receptor antagonist (AM-461): A patent evaluation of WO2011085033
    • Norman P. A novel DP2 receptor antagonist (AM-461): a patent evaluation of WO2011085033. Expert Opin Ther Pat 2011;21(12):1931-6
    • (2011) Expert Opin Ther Pat , vol.21 , Issue.12 , pp. 1931-1936
    • Norman, P.1
  • 42
    • 13944263887 scopus 로고    scopus 로고
    • Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist
    • DOI 10.1021/jm049036i
    • Ulven T, Kostenis E. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem 2005;48(4):897-900 (Pubitemid 40270433)
    • (2005) Journal of Medicinal Chemistry , vol.48 , Issue.4 , pp. 897-900
    • Ulven, T.1    Kostenis, E.2
  • 43
    • 76649106066 scopus 로고    scopus 로고
    • Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists
    • Grimstrup M, Receveur JM, Rist O, et al. Exploration of SAR features by modifications of thiazoleacetic acids as CRTH2 antagonists. Bioorg Med Chem Lett 2010;20(5):1638-41
    • (2010) Bioorg Med Chem Lett , vol.20 , Issue.5 , pp. 1638-1641
    • Grimstrup, M.1    Receveur, J.M.2    Rist, O.3
  • 44
    • 84855670521 scopus 로고    scopus 로고
    • Discovery of novel and potent CRTH2 antagonists
    • Ito S, Terasaka T, Zenkoh T, et al. Discovery of novel and potent CRTH2 antagonists. Bioorg Med Chem Lett 2012;22(2):1194-7
    • (2012) Bioorg Med Chem Lett , vol.22 , Issue.2 , pp. 1194-1197
    • Ito, S.1    Terasaka, T.2    Zenkoh, T.3
  • 45
    • 84878005145 scopus 로고    scopus 로고
    • Inhibition of antigen-induced airway inflammation and hyperresponsiveness in guinea pigs by a selective antagonist of chemoattractant receptor homologous molecule expressed on Th2 cells" (CRTH2)
    • Tasaki M, Kobayashi M, Tenda Y, et al. Inhibition of antigen-induced airway inflammation and hyperresponsiveness in guinea pigs by a selective antagonist of "chemoattractant receptor homologous molecule expressed on Th2 cells" (CRTH2). Eur J Pharm Sci 2013;49(3):434-40
    • (2013) Eur J Pharm Sci , vol.49 , Issue.3 , pp. 434-440
    • Tasaki, M.1    Kobayashi, M.2    Tenda, Y.3
  • 46
    • 84870551884 scopus 로고    scopus 로고
    • Development of a practical and scalable synthesis of a potent CRTH2 antagonist
    • Yoshida S, Yoshino T, Miyafuji M, et al. Development of a practical and scalable synthesis of a potent CRTH2 antagonist. Org. Process Res. Dev 2012;16(9):1544-51
    • (2012) Org. Process Res. Dev , vol.16 , Issue.9 , pp. 1544-1551
    • Yoshida, S.1    Yoshino, T.2    Miyafuji, M.3
  • 47
    • 84887046423 scopus 로고    scopus 로고
    • Efficacy and safety of AZD1981, a CRTH2 receptor antagonist, in patients with moderate to severe COPD
    • pii:S0954-6111
    • Snell N, Foster M, Vestbo J. Efficacy and safety of AZD1981, a CRTH2 receptor antagonist, in patients with moderate to severe COPD. Respir Med 2013;pii:S0954-6111
    • (2013) Respir Med
    • Snell, N.1    Foster, M.2    Vestbo, J.3
  • 48
    • 84875141481 scopus 로고    scopus 로고
    • Biochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma
    • Schmidt JA, Bell FM, Akam E, et al. Biochemical and pharmacological characterization of AZD1981, an orally available selective DP2 antagonist in clinical development for asthma. Br J Pharmacol 2013;168(7):1626-38
    • (2013) Br J Pharmacol , vol.168 , Issue.7 , pp. 1626-1638
    • Schmidt, J.A.1    Bell, F.M.2    Akam, E.3
  • 49
    • 84889820073 scopus 로고    scopus 로고
    • AstraZeneca plc, AZD1981 Available from
    • AstraZeneca plc, AZD1981. Available from: http://www.ncats.nih.gov/files/ AZD1981.pdf
  • 50
    • 84889834700 scopus 로고    scopus 로고
    • AstraZeneca plc, A Phase I, Single Centre, Double-blind, Randomised, Placebo-controlled,Parallel-group Study to Assess the Safety, Tolerability and Pharmacokinetics of Single Ascending Oral Doses of AZD8075 in Healthy Male Volunteers, Clinical Study Report September
    • AstraZeneca plc, A Phase I, Single Centre, Double-blind, Randomised, Placebo-controlled,Parallel-group Study to Assess the Safety, Tolerability and Pharmacokinetics of Single Ascending Oral Doses of AZD8075 in Healthy Male Volunteers, Clinical Study Report, September 2009
    • (2009)
  • 51
    • 84889875542 scopus 로고    scopus 로고
    • AstraZeneca plc, A Phase I, Single Centre, Double-blind, Randomised, Placebo-controlled, Parallel-group Study to Assess the Safety, Tolerability and Pharmacokinetics of Single Ascending Oral Doses of AZD5985 in Healthy Male Subjects, Clinical Study Report December 2009
    • AstraZeneca plc, A Phase I, Single Centre, Double-blind, Randomised, Placebo-controlled, Parallel-group Study to Assess the Safety, Tolerability and Pharmacokinetics of Single Ascending Oral Doses of AZD5985 in Healthy Male Subjects, Clinical Study Report, December 2009
  • 52
    • 84879587293 scopus 로고    scopus 로고
    • Identification of 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3- b] indol-5(2H)-yl)acetic acid (Setipiprant/ACT-129968), a Potent, selective and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist
    • Fretz H, Valdenaire A, Pothier J, et al. Identification of 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b] indol-5(2H)-yl)acetic acid (Setipiprant/ACT-129968), a Potent, selective and orally bioavailable chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonist. J Med Chem 2013;56(12):4899-911
    • (2013) J Med Chem , vol.56 , Issue.12 , pp. 4899-4911
    • Fretz, H.1    Valdenaire, A.2    Pothier, J.3
  • 53
    • 84872924984 scopus 로고    scopus 로고
    • Evolution of novel tricyclic CRTh2 receptor antagonists from a (E)-2-cyano-3-(1H-indol-3-yl)acrylamide scaffold
    • Valdenaire A, Pothier J, Renneberg D, et al. Evolution of novel tricyclic CRTh2 receptor antagonists from a (E)-2-cyano-3-(1H-indol-3-yl)acrylamide scaffold. Bioorg Med Chem Lett 2013;23(4):944-8
    • (2013) Bioorg Med Chem Lett , vol.23 , Issue.4 , pp. 944-948
    • Valdenaire, A.1    Pothier, J.2    Renneberg, D.3
  • 54
    • 84889824043 scopus 로고    scopus 로고
    • Actelion's novel crth2 antagonist meets primary endpoint in phase ii study in patients with seasonal allergic rhinitis
    • 23 may 2011
    • Actelion AG. Actelion's Novel Crth2 Antagonist Meets Primary Endpoint In Phase II Study In Patients With Seasonal Allergic Rhinitis, Press Release, 23 may 2011
    • Press Release
    • Actelion, A.G.1
  • 55
    • 79956066242 scopus 로고    scopus 로고
    • Discovery of AMG 853, a CRTH2 and DP dual antagonist
    • Liu J, Li A.-R, Wang Y, et al. Discovery of AMG 853, a CRTH2 and DP Dual Antagonist. ACS Med. Chem Lett 2011;2:326-30
    • (2011) ACS Med. Chem Lett , vol.2 , pp. 326-330
    • Liu, J.1    Li, A.-R.2    Wang, Y.3
  • 56
    • 84869113269 scopus 로고    scopus 로고
    • Predicting the drug interaction potential of AMG 853 a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors
    • Foti RS, Pearson JT, Wong SL, et al. Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors. Drug Metab Dispos 2012;40(12):2239-49
    • (2012) Drug Metab Dispos , vol.40 , Issue.12 , pp. 2239-2249
    • Foti, R.S.1    Pearson, J.T.2    Wong, S.L.3
  • 57
    • 84873407189 scopus 로고    scopus 로고
    • Safety and efficacy of the prostaglandin D2 receptor antagonist AMG 853 in asthmatic patients
    • Busse WW, Wenzel SE, Meltzer EO, et al. Safety and efficacy of the prostaglandin D2 receptor antagonist AMG 853 in asthmatic patients. J Allergy Clin Immunol 2013;131(2):339-45
    • (2013) J Allergy Clin Immunol , vol.131 , Issue.2 , pp. 339-345
    • Busse, W.W.1    Wenzel, S.E.2    Meltzer, E.O.3
  • 58
    • 84655161331 scopus 로고    scopus 로고
    • Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism
    • Wang Y, Fu Z, Schmitt M, et al. Optimization of phenylacetic acid derivatives for CRTH2 and DP selective antagonism. Bioorg Med Chem Lett 2012;22(1):367-70
    • (2012) Bioorg Med Chem Lett , vol.22 , Issue.1 , pp. 367-370
    • Wang, Y.1    Fu, Z.2    Schmitt, M.3
  • 63
    • 78650509769 scopus 로고    scopus 로고
    • Discovery of MK-7246 a selective CRTH2 antagonist for the treatment of respiratory diseases
    • Gallant M, Beaulieu C, Berthelette C, et al. Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases. Bioorg Med Chem Lett 2011;21(1):288-93
    • (2011) Bioorg Med Chem Lett , vol.21 , Issue.1 , pp. 288-293
    • Gallant, M.1    Beaulieu, C.2    Berthelette, C.3
  • 64
    • 84857809957 scopus 로고    scopus 로고
    • CRTH2 antagonist MK-7246: A synthetic evolution from discovery through development
    • Molinaro C, Bulger PG, Lee EE, et al. CRTH2 antagonist MK-7246: a synthetic evolution from discovery through development. J Org Chem 2012;77(5):2299-309
    • (2012) J Org Chem , vol.77 , Issue.5 , pp. 2299-2309
    • Molinaro, C.1    Bulger, P.G.2    Lee, E.E.3
  • 65
    • 78651341515 scopus 로고    scopus 로고
    • Pharmacological characterization of MK-7246 a potent and selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells) antagonist
    • Gervais FG, Sawyer N, Stocco R, et al. Pharmacological characterization of MK-7246, a potent and selective CRTH2 (chemoattractant receptor-homologous molecule expressed on T-helper type 2 cells) antagonist. Mol Pharmacol 2011;79(1):69-76
    • (2011) Mol Pharmacol , vol.79 , Issue.1 , pp. 69-76
    • Gervais, F.G.1    Sawyer, N.2    Stocco, R.3
  • 66
    • 84887994060 scopus 로고    scopus 로고
    • Pharmacological characterization of the late phase reduction in lung functions and correlations with microvascular leakage and lung edema in allergen-challenged Brown Norway rats
    • doi:pii: S1094-5539(13)00079-5. 10.1016/
    • Mauser PJ, House A, Jones H, et al. Pharmacological characterization of the late phase reduction in lung functions and correlations with microvascular leakage and lung edema in allergen-challenged Brown Norway rats. Pulm Pharmacol Ther 2013;doi:pii: S1094-5539(13)00079-5. 10.1016/
    • (2013) Pulm Pharmacol Ther
    • Mauser, P.J.1    House, A.2    Jones, H.3
  • 67
    • 84877585054 scopus 로고    scopus 로고
    • 2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists
    • Andrés M, Bravo M, Buil MA, et al. 2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists. Bioorg Med Chem Lett 2013;23(11):3349-53
    • (2013) Bioorg Med Chem Lett , vol.23 , Issue.11 , pp. 3349-3353
    • Andrés, M.1    Bravo, M.2    Buil, M.A.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.